(Z)-Leukadherin-1

CAS: 2055362-72-4 货号: L654782 分子式: C22H15NO4S2 分子量: 421.49
有货
级别和纯度: 10mM in DMSO
别名
(Z)-白细胞粘附素-1
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
L654782-1ml
期货 Stock Image
¥609.90
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概述


(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses

In Vitro

(Z)-Leukadherin-1 (ADH-503 free base; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b + cells and subsets of CD11b + monocytes, granulocytes, eosinophils, and macrophages. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(Z)-Leukadherin-1 (ADH-503 free base; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival . (Z)-Leukadherin-1 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras G12D /p53 flox/flox ] Dosage: 30, 60, or 120 mg/kg Administration: Oral gavage; 60 days Result: Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival. Animal Model: Male rats Dosage: 30, 100 mg/kg (Pharmacokinetic Analysis) Administration: Oral gavage twice a day; on days 1 and 5 Result: Had the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/ml and AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.

IC50& Target:CD11b

规格

别名
(Z)-白细胞粘附素-1
规格或纯度
10mM in DMSO
英文名称
(Z)-Leukadherin-1
生化机理
(Z)-Leukadherin-1(ADH-503 游离碱)是一种口服活性异构 CD11b 激动剂。(Z)-Leukadherin-1能使肿瘤相关巨噬细胞重新极化,减少肿瘤浸润性免疫抑制髓系细胞的数量,并增强肿瘤相关巨噬细胞的活性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC=C(C=C1)CN2C(=O)/C(=C/C3=CC=C(O3)C4=CC=C(C=C4)C(=O)O)/SC2=S
MeSH Entry Terms
leukadherin-1
分子量
421.49
Reaxy-Rn
28009878
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28009878&ln=

高级数据

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